PAC3421 Study Guide - Final Guide: 2-Cyanoguanidine, Aromatic Amine, Ranitidine
23 Jun 2018
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Treatment of Otitis Media:
a) Analgesics (e.g. paracetamol or ibuprofen)
b) Antibiotics
a. Only used in children under certain circumstances (refer notes)
b. First-line: Amoxycillin, augmentin, cefuroxime
Respiratory Pathophysiology:
Using the knowledge of absorption, metabolism, pharmacology and medicinal chemistry can you explain
why bambuterol it might be useful for treating asthma and COPD?
Absorption:
The entire molecule masks the OH groups of the catechol as esters to increase lipophilicity of
molecule to aid absorption
This enables better absorption across membranes
Metabolism:
Susceptible to hydrolysis of two ester groups (or esterase activity) to reveal catechol group
Catechol group is likely to be beta2 agonist so useful for asthma treatment
Catechol group is liable to metabolism by COMT and MAO
Medicinal chemistry:
Bulky/large alkyl N-substituent gives rise to beta-adrenoceptor selectivity
Ionisable amine group - Ionised tertiary nitrogen will interact with aspartic acid in the binding site
Pharmacology:
The molecule provides good duration of action (about 8 hours)
Beta2-adrenoceptor agonist on bronchial smooth muscles allows bronchodilatation, increasing
airway diameter, airflow not obstructed, facilitating efficient gaseous exchange, preventing
breathing difficulties/symptoms
find more resources at oneclass.com
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Document Summary
Treatment of otitis media: analgesics (e. g. paracetamol or ibuprofen, antibiotics, only used in children under certain circumstances (refer notes, first-line: amoxycillin, augmentin, cefuroxime. The entire molecule masks the oh groups of the catechol as esters to increase lipophilicity of molecule to aid absorption. Susceptible to hydrolysis of two ester groups (or esterase activity) to reveal catechol group. Catechol group is likely to be beta2 agonist so useful for asthma treatment. Catechol group is liable to metabolism by comt and mao. Bulky/large alkyl n-substituent gives rise to beta-adrenoceptor selectivity. Ionisable amine group - ionised tertiary nitrogen will interact with aspartic acid in the binding site. The molecule provides good duration of action (about 8 hours) Beta2-adrenoceptor agonist on bronchial smooth muscles allows bronchodilatation, increasing airway diameter, airflow not obstructed, facilitating efficient gaseous exchange, preventing breathing difficulties/symptoms. General pharmacological class of medicinal agents does tiotropium belong to: (long-acting) muscarinic antagonists.
